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► Med - Pharmacology > Drug Transporters > Flashcards

Drug Transporters Flashcards

1
Q

What happens when there is a decrease in the uptake or the efflux of drug in the liver or kidney?

A

It will lead to increased plasma concentration of the drug which can lead to increased toxicity.

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2
Q

What happens where there is an increase in the uptake and a decrease in the efflux in the target organ for the drug?

A

It will lead to increased concentration of drug in the target organ and increased toxicity.

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3
Q

What happens when there is an inhibition of transport of drugs?

A

The concentration in the blood will be increased which can lead to increased toxicity.

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4
Q

How do drug-drug reactions impact transport?

A

Drug B can block a transporter for Drug A, causing Drug A to build up in the plasma and so the high concentration of Drug A can lead to toxicity and/or decrease the efficacy of the drug as it isn’t reaching the target organ.

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5
Q

What are the transporters of the solute carrier superfamily (SLC)?

A

OAT
OATP
OCT
MATE

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6
Q

What are the transporters of the ATP-binding cassette superfamily (ABC)?

A

P-gp/MDR1
BCRP
MRP

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7
Q

OAT

A

Organic Anion Transporter

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8
Q

How does OAT transport?

A

Uptake

Antiports an organic anion and a-ketoglutarate

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9
Q

Where is OAT found?

A

Liver

PT of kidney

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10
Q

What does OAT transport?

A

Low MW organic anions

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11
Q

How does methotrexate and NSAIDs interact with OAT?

A

NSAIDs block the activity of OAT and methotrexate cannot be taken into the kidney leading to methotrexate toxicity

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12
Q

How is probenecid used with cidefovir and OAT?

A

Probenecid prevents Cidefovir renal uptake which blocks cidefovir-induced nephrotoxicity

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13
Q

OATP

A

Organic Anion Transporter Polypeptides

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14
Q

How does OATP transport?

A

Antiprotons organic anion and HCO3-

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15
Q

Where is OATP found?

A

Gut
Liver
Kidney PT

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16
Q

What does OATP transport?

A

Uptake

Amphipathic anions of MW > 350 Da

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17
Q

What are the problems with OATP SNPs and statins?

A

Some OATP polymorphisms lead to decreased statin transport which reduces their efficacy and increases their toxicity

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18
Q

What is the effect of cyclosporin on OATP and statins?

A

Cyclosporin block OATP, which blocks STATIN uptake and causes STATIN toxicity

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19
Q

OCT

A

Organic Cation Transporter

20
Q

How does OCT transport?

A

Uptake

Simple facilitated diffusion of organic cations

21
Q

Where is OCT found?

A

Gut
Liver
Kidney

22
Q

What does OCT transport?

A

Small cations

23
Q

MATE

A

Multidrug and Toxin Extrusion Transporter

24
Q

How does MATE transport?

A

Efflux

Antiports H+ and cationic drugs

25
Q

Where is MATE found?

A

Liver

Kidney

26
Q

What does MATE transport?

A

Main role is in secretion of the OCT substrates

27
Q

What can SNPs of OCT/MATE cause?

A

It can cause the loss of either of these transporter’s activities which will lead to increased drug toxicity

28
Q

How does cimetidine affect OCT/MATE and procainamide?

A

Cimetidine blocks OCT-mediated renal uptake of many drugs like procainaminde which blocks their elimination and increases their plasma concentration

29
Q

How does cimetidine affect OCT/MATE and cisplatin?

A

Cimetidine blocks OCT uptake of cisplatin and prevents the nephrotoxic effects of cisplatin

30
Q

P-gp/MRD1

A

P-glycoprotein/Multidrug Resistant Protein 1

31
Q

How does P-gp/MRD1 transport?

A

Efflux

Active Transport

32
Q

Where is P-gp/MRD1 found?

A

Intestine
Kidney
Liver

33
Q

What does P-gp/MRD1 transport?

A

Bulky hydrophobic neutral or positively charged molecules

34
Q

How does cyclosporin affect P-gp/MRD1 and digoxin?

A

Cyclosporin inhibits P-gp-mediated elimination of digoxin which increases availability and toxicity as digoxin has a narrow therapeutic range

35
Q

How do rifampicin and St. John’s Wort affect P-gp?

A

Both induce Pg-p and will lead to increased drug efflux, leading to decreased drug efficacy

36
Q

How does cyclosporin affect loperamide and P-gp?

A

Cyclosporin inhibits P-gp, which will enhance CNS accessibility by overcoming BBB and allow loperamide to pass the BBB and enter the CNS leading to respiratory depression

37
Q

How do tumor cells use P-gp?

A

Tumor cells up regulate P-gp by up regulating it which allow them to have high efflux of anti-cancer drugs

38
Q

BCRP

A

Breast Cancer Resistant Protein

39
Q

What is the general function of BCRP?

A

Concentrates breast milk

40
Q

Where is BCRP found?

A

Breast
Gut
Liver
BBB

41
Q

What does BCRP transport?

A

Transports neutral and negatively charged compounds like statins

42
Q

MRP

A

Multidrug Resistant Protein

43
Q

Where is MRP found?

A

Many tissues

44
Q

What does MRP transport?

A

Transports positive amphipathic molecules

45
Q

How is the BBB maintained?

A

It is maintained via an ABC transporter that actively pumps compounds like drugs out to the blood and keeps them out of the CNS.

► Med - Pharmacology (74 decks)

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